D-ring modified novel isosteviol derivatives: design, synthesis and cytotoxic activity evaluation

  • Bioorg Med Chem Lett. 2012 Sep 15;22(18):5827-32. doi: 10.1016/j.bmcl.2012.07.083.
Tao Zhang  1 ,  Li-Hui Lu ,  Hao Liu ,  Jun-Wei Wang ,  Rui-Xue Wang ,  Yun-Xiao Zhang ,  Jing-Chao Tao
Affiliations
  • 1. College of Chemistry and Molecular Engineering, New Drug Research & Development Center, Zhengzhou University, 75 Daxue Road, Zhengzhou 450052, PR China.
PMID: 22901386 DOI: 10.1016/j.bmcl.2012.07.083
Abstract

A series of polyhydric, amino alcohol and tricyclic derivatives were facilely synthesized by D-ring modification of isosteviol. These compounds were screened for their cytotoxic activities against four human tumor cell lines in vitro. Among them, the 15-α-aminomethyl-16-β-hydroxyl isosteviol 23 exhibits significant cytotoxicity superior to the positive control (cisplatin) against EC9706, PC-3 and HCT-116 cell lines.